Synthesis and Biological Evaluation of Quinazoline-4-thiones

Several 2,2-dimethyl-3-phenyl-1,2-dihydroquinazoline-4(3H)-thiones and 2-methyl-3-phenylquinazoline-4(3H)-thiones were synthesized and tested for their antimycobacterial, photosynthesis-inhibiting, and antialgal activity. Antimycobacterially active compounds were found among the 6-chloro substituted...

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Published in:Molecules (Basel, Switzerland) Switzerland), 2003-11, Vol.8 (11), p.756-769
Main Authors: Kubicová, Lenka, Šustr, Martin, Kráľová, Katarína, Chobot, Vladimír, Vytlačilová, Jitka, Jahodář, Luděk, Vuorela, Pia, Macháček, Miloš, Kaustová, Jarmila
Format: Article
Language:English
Subjects:
alga
Artemia salina
Bioassays
Chloroplasts
mycobacteria
Pharmacy
Photosynthesis
photosynthesis-inhibiting activity
Quinazoline-4-thiones
toxicological screening
Tuberculosis
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Summary:Several 2,2-dimethyl-3-phenyl-1,2-dihydroquinazoline-4(3H)-thiones and 2-methyl-3-phenylquinazoline-4(3H)-thiones were synthesized and tested for their antimycobacterial, photosynthesis-inhibiting, and antialgal activity. Antimycobacterially active compounds were found among the 6-chloro substituted compounds. 6-Chloro-3-(4-isopropylphenyl)-2-methylquinazoline-4(3H)-thione exhibited higher activity than the isoniazid standard against Mycobacterium avium and M. kansasii. Most of the compounds possessed photosynthesis-inhibiting activity. 6-Chloro-2,2-dimethyl-3-phenyl-1,2-dihydroquinazoline-4(3H)-thione and its 3´-chloro- and 3´,4´-dichloro analogs were most effective in the inhibition of oxygen evolution rate in spinach chloroplasts. Of compounds selected for toxicological screening, 6-chloro-3-(4-isopropylphenyl)-2-methyl-quinazoline-4(3H)-thione was the only one active in the brine shrimp bioassay.
ISSN:1420-3049
1420-3049
DOI:10.3390/81100756